Sabizabulin VERU-111; ABI-231|cas:1332881-26-1|西域试剂

Sabizabulin VERU-111; ABI-231,98.75%

产品编号：Bellancom-120599| CAS NO：1332881-26-1| 分子式：C₂₁H₁₉N₃O₄| 分子量：377.39

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货号	价格	库存与货期
Bellancom-120599	￥4500.00	杭州北京（现货）
Bellancom-120599	￥6950.00	杭州北京（现货）
Bellancom-120599	￥13160.00	杭州北京（现货）

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Sabizabulin VERU-111; ABI-231

产品介绍

VERU-111 (ABI-231) 是一种高效、口服可利用 α/β 微管蛋白 (tubulin) 抑制剂，具有很强的抗增殖活性，对黑素瘤和前列腺癌细胞系作用的平均 IC₅₀ 值为 5.2 nM。VERU-111 (ABI-231) 通过靶向 HPV E6 和 E7 抑制肿瘤生长和转移表型，有潜力用于前列腺癌的研究。

生物活性

VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC₅₀ of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.

体外研究

VERU-111 (2.5-80 nM; 24-48 hours) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner (24 hours: IC₅₀s of 25, 35 and 35 nM, respectively; 48 hours: IC₅₀s of 11.8, 15.5, and 25 nM, respectively)^[4].
VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner^[4].
VERU-111 (5-20 nM; 24 hours) shows dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9, induces the expression of Bax and Bad, and inhibits the expression of Bcl-2 and Bcl-xl proteins in both AsPC-1 and Panc-1 cells^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:	Panc-1, AsPC-1, HPAF-II cells
Concentration:	2.5, 5, 10, 20, 40, 80 nM
Incubation Time:	24, 48 hours
Result:	Inhibited the growth of PanCa cells in a dose and time-dependent manner. The IC₅₀ of VERU-111 was 25, 35 and 35 nM in Panc-1, AsPC-1 and HPAF-II, respectively after 24 h treatment, while 48 h post-treatment it was 11.8, 15.5, and 25 nM.

Apoptosis Analysis^[4]

Cell Line:	Panc-1, AsPC-1 cells
Concentration:	5, 10, 20 nM
Incubation Time:	24 hours
Result:	Arrested Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner.

Western Blot Analysis^[4]

Cell Line:	AsPC-1 and Panc-1 cells
Concentration:	5, 10, 20 nM
Incubation Time:	24 hours
Result:	Dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9 in both AsPC-1 and Panc-1 cells. Induces the expression of Bax and Bad and inhibited the expression of Bcl-2 and Bcl-xl proteins.

体内研究
(In Vivo)

VERU-111 (50 μg/mouse; intra-tumorally; 3 times per week for 3 weeks) effectively inhibits tumor growth as compared to vehicle-treated group. None of the mouse showed any apparent toxicity as constant increase of body weight in VERU-111 treated mice^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female athymic nude mice (bearing AsPC-1 cells)
Dosage:	50 μg/mouse
Administration:	Intra-tumorally; 3 times per week for 3 weeks
Result:	Effectively inhibited tumor growth.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female athymic nude mice (bearing AsPC-1 cells)
Dosage:	50 μg/mouse
Administration:	Intra-tumorally; 3 times per week for 3 weeks
Result:	Effectively inhibited tumor growth.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female athymic nude mice (bearing AsPC-1 cells)
Dosage:	50 μg/mouse
Administration:	Intra-tumorally; 3 times per week for 3 weeks
Result:	Effectively inhibited tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (53.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6498 mL	13.2489 mL	26.4978 mL
5 mM	0.5300 mL	2.6498 mL	5.2996 mL
10 mM	0.2650 mL	1.3249 mL	2.6498 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (5.30 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明